Uses
XRK3F2 is an inhibitor of p62 (Sequestosome-1)-ZZ/ domain.
Biological Activity
XRK3F2 is a p62-ZZ inhibitor that blunts multiple myeloma (MM)-induced Runx2 inhibition in vitro and induces new bone formation and remodeling in the presence of tumors in vivo.
in vivo
In vivo, XRK3F2 induces new bone formation and remodeling in tumors. The half-life of it in mice was 10.3 hours. In bone with multiple myeloma, it induced significant local new bone formation, but not in mice not directly inoculated with multiple myeloma cells.
References
[1] Adamik J, et al. XRK3F2 Inhibition of p62-ZZ Domain Signaling Rescues Myeloma-Induced GFI1-Driven Epigenetic Repression of the Runx2 Gene in Pre-osteoblasts to Overcome Differentiation Suppression. Front Endocrinol (Lausanne). 2018 Jun 29;9:344. DOI:
10.3389/fendo.2018.00344